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Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, spect and pet imaging

United States Patent

5,639,879
June 17, 1997
View the Complete Patent at the US Patent & Trademark Office
Brookhaven National Laboratory - Visit the Office of Technology Commercialization and Partnerships Website
A simple method for the synthesis of 1,4,7, 10-tetraazacyclododecane N,N'N",N'"-tetraacetic acid and 1,4,8,11-tetraazacyclotetradecane N,N',N",N'"-tetraacetic acid involves cyanomethylating 1,4,7, 10-tetraazacyclododecane or 1,4,8,11-tetraazacyclotetradecane to form a tetranitrile and hydrolyzing the tetranitrile. These macrocyclic compounds are functionalized through one of the carboxylates and then conjugated to various biological molecules including monoclonal antibodies. The resulting conjugated molecules are labeled with radiometals for SPECT and PET imaging and for radiotherapy.
Mease; Ronnie C. (Fairfax, VA), Mausner; Leonard F. (Stony Brook, NY), Srivastava; Suresh C. (Setauket, NY)
Associated Universities, Inc. (Washington, DC)
08/ 382,522
February 2, 1995
This invention was made with government support under contract number DE-AC02-76CH00016 Between the U.S. Department of Energy and Associated Universities and NIH Grant CA-51958. The government has certain rights in the invention.